Urease-IN-24
Urease-IN-24 is a cryptococcal urease inhibitor with a IC50 of 89.96 nM and a Ki of 64.3 nM. Urease-IN-24 acts as a competitive nickel-coordinating inhibitor that coordinates with the nickel center at the catalytic site of the enzyme via its carbonyl group. Urease-IN-24 reduces the capsule thickness of Cryptococcus neoformans and Cryptococcus gattii, increases cell membrane permeability, and inhibits melanin production. Urease-IN-24 exhibits fungicidal activity against Cryptococcus species. Urease-IN-24 can be used in the research of cryptococcosis.
For research use only. We do not sell to patients.
- CAS No.: 2243516-99-4
- Formula: C14H16N2O3Se
- Molecular Weight:339.25
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Urease-IN-24 (AF57) (48 h) inhibits planktonic growth and cell urease activity of clinical isolates of Cryptococcus neoformans and Cryptococcus gattii in RPMI and Christensen media, with IC50 values ranging from ≤0.1-6 μM, IC90 values ranging from 0.3-12 μM, ICURE values ranging from ≤0.1-1.5 μM, and MFC values ranging from 0.3-48 μM, depending on the species and medium[1].
Urease-IN-24 inhibits biofilm formation and growth of dispersed biofilm cells of Cryptococcus neoformans H99 and Cryptococcus gattii R265 with IC90 values of 3-6 μM and DMIC values of 6 μM, but does not inhibit metabolic activity of preformed mature biofilm sessile cells at concentrations up to 378 μM[1].
Urease-IN-24 (3 μM; 48 h) significantly reduces capsule thickness of Cryptococcus neoformans H99 and Cryptococcus gattii R265[1].
Urease-IN-24 (3-6 μM; 96 h) completely inhibits melanin production in Cryptococcus neoformans H99 and Cryptococcus gattii R265 after 96 h of incubation on L-DOPA-supplemented medium[1].
Urease-IN-24 (3-48 μM; 0-72 h) exhibits fungicidal activity against Cryptococcus neoformans H99 and Cryptococcus gattii R265, reducing viability to undetectable levels within 12 h at 2×IC90 (12 μM for H99, 6 μM for R265)[1].
Urease-IN-24 (6-192 μM; 12 h) significantly increases plasma membrane permeability of Cryptococcus neoformans H99 and Cryptococcus gattii R265[1].
Urease-IN-24 (0.06-1000 ng/mL; 10 min) potently inhibits Cryptococcus neoformans urease in a cell-free assay with a IC50 of 89.96 nM and acts as a competitive inhibitor with a Ki of 64.3 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:larvae (2.0-2.5 cm length, 150-200 mg body mass)[1]
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Dosage:100 mg/kg
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Administration:injection into last left pro-leg; single dose
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Result:Resulted in 100% larval survival over 5 days.
Maintained high health index scores comparable to PBS and DMSO control groups.
Chemical Information
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CAS No. 2243516-99-4
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Molecular Weight 339.25
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Formula C14H16N2O3Se
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SMILES
CCOC(C1=C(C)NC(NC1C2=CC(O)=CC=C2)=[Se])=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)